title: The structure of a new cardenolide diglycoside and the biological activities of eleven cardenolide diglycosides from Nerium oleander.
abstract: A new cardenolide diglycoside (1) was isolated from Nerium oleander together with ten known cardenolide diglycosides 2-11. The structure of compound 1 was established on the basis of their spectroscopic data. The in vitro anti-inflammatory activity of compounds 1-11 was examined on the basis of inhibitory activity against the induction of the intercellular adhesion molecule-1 (ICAM-1). Compounds 2-5 were active at an IC(50) value of less than 0.8 µM. The cytotoxicity of compounds 1-11 was evaluated against three human cell lines normal human fibroblast cells (WI-38), malignant tumor cells induced from WI-38 (VA-13), and human liver tumor cells (HepG2). Compound 3 was active toward VA-13 cells, and compounds 2-5 were active toward HepG2 cells at IC(50) values of less than 1.3 µM. The multidrug resistance (MDR)-reversal activity of compounds 1-11 was evaluated on the basis of the amount of calcein in MDR human ovarian cancer 2780AD cells in the presence of each compound. Compounds 1 and 8 showed moderate effects on calcein accumulation.
authors.affiliation: College of Chemistry and Chemical Engineering, Qiqihar University, 30 Wenhuadajie, Qiqihar, Heilongjiang Province, China. mingzhaoqd@gmail.com
authors.forename: Ming
authors.initials: M
authors.lastname: Zhao
authors.forename: Liming
authors.initials: L
authors.lastname: Bai
authors.forename: Asami
authors.initials: A
authors.lastname: Toki
authors.forename: Ryo
authors.initials: R
authors.lastname: Hasegawa
authors.forename: Jun-ichi
authors.initials: J
authors.lastname: Sakai
authors.forename: Toshiaki
authors.initials: T
authors.lastname: Hasegawa
authors.forename: Hirotsugu
authors.initials: H
authors.lastname: Ogura
authors.forename: Takao
authors.initials: T
authors.lastname: Kataoka
authors.forename: Yuhua
authors.initials: Y
authors.lastname: Bai
authors.forename: Mariko
authors.initials: M
authors.lastname: Ando
authors.forename: Katsutoshi
authors.initials: K
authors.lastname: Hirose
authors.forename: Masayoshi
authors.initials: M
authors.lastname: Ando
mesh_terms: D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000302:isolation & purification / Q000633:toxicity; D002298:Cardenolides / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D045744:Cell Line, Tumor; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D005260:Female; D005452:Fluoresceins / Q000378:metabolism; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D030007:Nerium / Q000737:chemistry*; D010051:Ovarian Neoplasms / Q000188:drug therapy
chemical_list: D000893:Anti-Inflammatory Agents; D000972:Antineoplastic Agents, Phytogenic; D002298:Cardenolides; D005452:Fluoresceins; C007740:fluorexon